CN1960731B - 调节炎性和转移过程的方法 - Google Patents
调节炎性和转移过程的方法 Download PDFInfo
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- CN1960731B CN1960731B CN2005800095231A CN200580009523A CN1960731B CN 1960731 B CN1960731 B CN 1960731B CN 2005800095231 A CN2005800095231 A CN 2005800095231A CN 200580009523 A CN200580009523 A CN 200580009523A CN 1960731 B CN1960731 B CN 1960731B
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- benzimidazol
- substituted
- ylamino
- unsubstituted
- azabicyclo
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- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
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- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 description 1
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- 230000001404 mediated effect Effects 0.000 description 1
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- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 1
- NSPJNIDYTSSIIY-UHFFFAOYSA-N methoxy(methoxymethoxy)methane Chemical compound COCOCOC NSPJNIDYTSSIIY-UHFFFAOYSA-N 0.000 description 1
- LNDSAJQLFLRWTE-SANMLTNESA-N methyl 3-[4-[[(3R)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1H-benzimidazol-2-yl)-2-oxo-1H-quinolin-6-yl]benzoate Chemical compound COC(=O)c1cccc(c1)-c1ccc2[nH]c(=O)c(-c3nc4ccccc4[nH]3)c(N[C@H]3CN4CCC3CC4)c2c1 LNDSAJQLFLRWTE-SANMLTNESA-N 0.000 description 1
- IDOWGLKEVBMZRK-DEOSSOPVSA-N methyl 3-[4-[[(3R)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1H-benzimidazol-2-yl)-5-fluoro-2-oxo-1H-quinolin-6-yl]benzoate Chemical compound COC(=O)c1cccc(c1)-c1ccc2[nH]c(=O)c(-c3nc4ccccc4[nH]3)c(N[C@H]3CN4CCC3CC4)c2c1F IDOWGLKEVBMZRK-DEOSSOPVSA-N 0.000 description 1
- WKKIAILNSMGTCG-SANMLTNESA-N methyl 3-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-2-oxo-1h-quinolin-7-yl]benzoate Chemical compound COC(=O)C1=CC=CC(C=2C=C3NC(=O)C(C=4NC5=CC=CC=C5N=4)=C(N[C@@H]4C5CCN(CC5)C4)C3=CC=2)=C1 WKKIAILNSMGTCG-SANMLTNESA-N 0.000 description 1
- FTAHGDIDPGHHNL-SANMLTNESA-N methyl 3-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-7-chloro-2-oxo-1h-quinolin-6-yl]benzoate Chemical compound COC(=O)C1=CC=CC(C=2C(=CC=3NC(=O)C(C=4NC5=CC=CC=C5N=4)=C(N[C@@H]4C5CCN(CC5)C4)C=3C=2)Cl)=C1 FTAHGDIDPGHHNL-SANMLTNESA-N 0.000 description 1
- HAKRHVMKPNVIIF-SANMLTNESA-N methyl 3-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-7-fluoro-2-oxo-1h-quinolin-6-yl]benzoate Chemical compound COC(=O)C1=CC=CC(C=2C(=CC=3NC(=O)C(C=4NC5=CC=CC=C5N=4)=C(N[C@@H]4C5CCN(CC5)C4)C=3C=2)F)=C1 HAKRHVMKPNVIIF-SANMLTNESA-N 0.000 description 1
- WKKIAILNSMGTCG-AREMUKBSSA-N methyl 3-[4-[[(3s)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-2-oxo-1h-quinolin-7-yl]benzoate Chemical compound COC(=O)C1=CC=CC(C=2C=C3NC(=O)C(C=4NC5=CC=CC=C5N=4)=C(N[C@H]4C5CCN(CC5)C4)C3=CC=2)=C1 WKKIAILNSMGTCG-AREMUKBSSA-N 0.000 description 1
- LZGAHPYXJJJEMB-SANMLTNESA-N methyl 3-amino-4-[4-[[(3R)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1H-benzimidazol-2-yl)-2-oxo-1H-quinolin-6-yl]benzoate Chemical compound COC(=O)c1ccc(c(N)c1)-c1ccc2[nH]c(=O)c(-c3nc4ccccc4[nH]3)c(N[C@H]3CN4CCC3CC4)c2c1 LZGAHPYXJJJEMB-SANMLTNESA-N 0.000 description 1
- BCCHGXPLQSUIOJ-DEOSSOPVSA-N methyl 3-amino-4-[4-[[(3R)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1H-benzimidazol-2-yl)-5-fluoro-2-oxo-1H-quinolin-6-yl]benzoate Chemical compound COC(=O)c1ccc(c(N)c1)-c1ccc2[nH]c(=O)c(-c3nc4ccccc4[nH]3)c(N[C@H]3CN4CCC3CC4)c2c1F BCCHGXPLQSUIOJ-DEOSSOPVSA-N 0.000 description 1
- SQTKTVRKQUQSLX-SANMLTNESA-N methyl 3-amino-4-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-2-oxo-1h-quinolin-7-yl]benzoate Chemical compound NC1=CC(C(=O)OC)=CC=C1C1=CC=C(C(N[C@@H]2C3CCN(CC3)C2)=C(C=2NC3=CC=CC=C3N=2)C(=O)N2)C2=C1 SQTKTVRKQUQSLX-SANMLTNESA-N 0.000 description 1
- GVWINYZJXSKHRP-SANMLTNESA-N methyl 3-amino-4-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-7-chloro-2-oxo-1h-quinolin-6-yl]benzoate Chemical compound NC1=CC(C(=O)OC)=CC=C1C(C(=C1)Cl)=CC2=C1NC(=O)C(C=1NC3=CC=CC=C3N=1)=C2N[C@@H]1C(CC2)CCN2C1 GVWINYZJXSKHRP-SANMLTNESA-N 0.000 description 1
- PNSNBBQPVGSTKA-SANMLTNESA-N methyl 3-amino-4-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-7-fluoro-2-oxo-1h-quinolin-6-yl]benzoate Chemical compound NC1=CC(C(=O)OC)=CC=C1C(C(=C1)F)=CC2=C1NC(=O)C(C=1NC3=CC=CC=C3N=1)=C2N[C@@H]1C(CC2)CCN2C1 PNSNBBQPVGSTKA-SANMLTNESA-N 0.000 description 1
- KKDYJFMDLOYXCP-SANMLTNESA-N methyl 4-[4-[[(3R)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1H-benzimidazol-2-yl)-2-oxo-1H-quinolin-6-yl]benzoate Chemical compound COC(=O)c1ccc(cc1)-c1ccc2[nH]c(=O)c(-c3nc4ccccc4[nH]3)c(N[C@H]3CN4CCC3CC4)c2c1 KKDYJFMDLOYXCP-SANMLTNESA-N 0.000 description 1
- SZQNCJQAPHAGRH-DEOSSOPVSA-N methyl 4-[4-[[(3R)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1H-benzimidazol-2-yl)-5-fluoro-2-oxo-1H-quinolin-6-yl]benzoate Chemical compound COC(=O)c1ccc(cc1)-c1ccc2[nH]c(=O)c(-c3nc4ccccc4[nH]3)c(N[C@H]3CN4CCC3CC4)c2c1F SZQNCJQAPHAGRH-DEOSSOPVSA-N 0.000 description 1
- NXOKSOCUKUJLGL-SANMLTNESA-N methyl 4-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-2-oxo-1h-quinolin-7-yl]benzoate Chemical compound C1=CC(C(=O)OC)=CC=C1C1=CC=C(C(N[C@@H]2C3CCN(CC3)C2)=C(C=2NC3=CC=CC=C3N=2)C(=O)N2)C2=C1 NXOKSOCUKUJLGL-SANMLTNESA-N 0.000 description 1
- FXNHJALUCDRYOR-SANMLTNESA-N methyl 4-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-7-chloro-2-oxo-1h-quinolin-6-yl]benzoate Chemical compound C1=CC(C(=O)OC)=CC=C1C(C(=C1)Cl)=CC2=C1NC(=O)C(C=1NC3=CC=CC=C3N=1)=C2N[C@@H]1C(CC2)CCN2C1 FXNHJALUCDRYOR-SANMLTNESA-N 0.000 description 1
- AFLHTAOSKNVOPS-SANMLTNESA-N methyl 4-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-7-fluoro-2-oxo-1h-quinolin-6-yl]benzoate Chemical compound C1=CC(C(=O)OC)=CC=C1C(C(=C1)F)=CC2=C1NC(=O)C(C=1NC3=CC=CC=C3N=1)=C2N[C@@H]1C(CC2)CCN2C1 AFLHTAOSKNVOPS-SANMLTNESA-N 0.000 description 1
- JKIWBEFVMOZPLU-SANMLTNESA-N methyl 4-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-7-methoxy-2-oxo-1h-quinolin-6-yl]benzoate Chemical compound C1=CC(C(=O)OC)=CC=C1C(C(=C1)OC)=CC2=C1NC(=O)C(C=1NC3=CC=CC=C3N=1)=C2N[C@@H]1C(CC2)CCN2C1 JKIWBEFVMOZPLU-SANMLTNESA-N 0.000 description 1
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- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- CPZBTYRIGVOOMI-UHFFFAOYSA-N methylsulfanyl(methylsulfanylmethoxy)methane Chemical compound CSCOCSC CPZBTYRIGVOOMI-UHFFFAOYSA-N 0.000 description 1
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- RVNGCCHKHYZBQH-KOSHJBKYSA-N n-[(3r)-1-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-6-fluoro-2-oxo-1h-quinolin-7-yl]pyrrolidin-3-yl]acetamide Chemical compound C1[C@H](NC(=O)C)CCN1C(C(=C1)F)=CC2=C1C(N[C@@H]1C3CCN(CC3)C1)=C(C=1NC3=CC=CC=C3N=1)C(=O)N2 RVNGCCHKHYZBQH-KOSHJBKYSA-N 0.000 description 1
- RVNGCCHKHYZBQH-HOYKHHGWSA-N n-[(3r)-1-[4-[[(3s)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-6-fluoro-2-oxo-1h-quinolin-7-yl]pyrrolidin-3-yl]acetamide Chemical compound C1[C@H](NC(=O)C)CCN1C(C(=C1)F)=CC2=C1C(N[C@H]1C3CCN(CC3)C1)=C(C=1NC3=CC=CC=C3N=1)C(=O)N2 RVNGCCHKHYZBQH-HOYKHHGWSA-N 0.000 description 1
- RVNGCCHKHYZBQH-UUOWRZLLSA-N n-[(3s)-1-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-6-fluoro-2-oxo-1h-quinolin-7-yl]pyrrolidin-3-yl]acetamide Chemical compound C1[C@@H](NC(=O)C)CCN1C(C(=C1)F)=CC2=C1C(N[C@@H]1C3CCN(CC3)C1)=C(C=1NC3=CC=CC=C3N=1)C(=O)N2 RVNGCCHKHYZBQH-UUOWRZLLSA-N 0.000 description 1
- RVNGCCHKHYZBQH-MHECFPHRSA-N n-[(3s)-1-[4-[[(3s)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-6-fluoro-2-oxo-1h-quinolin-7-yl]pyrrolidin-3-yl]acetamide Chemical compound C1[C@@H](NC(=O)C)CCN1C(C(=C1)F)=CC2=C1C(N[C@H]1C3CCN(CC3)C1)=C(C=1NC3=CC=CC=C3N=1)C(=O)N2 RVNGCCHKHYZBQH-MHECFPHRSA-N 0.000 description 1
- GLAFLDLQNFJJRW-XLDIYJRPSA-N n-[1-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-6-fluoro-2-oxo-1h-quinolin-7-yl]pyrrolidin-3-yl]-2,2,2-trifluoroacetamide Chemical compound FC1=CC=2C(N[C@@H]3C4CCN(CC4)C3)=C(C=3NC4=CC=CC=C4N=3)C(=O)NC=2C=C1N1CCC(NC(=O)C(F)(F)F)C1 GLAFLDLQNFJJRW-XLDIYJRPSA-N 0.000 description 1
- GLAFLDLQNFJJRW-VXNXSFHZSA-N n-[1-[4-[[(3s)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-6-fluoro-2-oxo-1h-quinolin-7-yl]pyrrolidin-3-yl]-2,2,2-trifluoroacetamide Chemical compound FC1=CC=2C(N[C@H]3C4CCN(CC4)C3)=C(C=3NC4=CC=CC=C4N=3)C(=O)NC=2C=C1N1CCC(NC(=O)C(F)(F)F)C1 GLAFLDLQNFJJRW-VXNXSFHZSA-N 0.000 description 1
- LBWFXVZLPYTWQI-IPOVEDGCSA-N n-[2-(diethylamino)ethyl]-5-[(z)-(5-fluoro-2-oxo-1h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide;(2s)-2-hydroxybutanedioic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O.CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C LBWFXVZLPYTWQI-IPOVEDGCSA-N 0.000 description 1
- TVOCUVRCGNRVTP-QHCPKHFHSA-N n-[2-[[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-6-fluoro-2-oxo-1h-quinolin-7-yl]amino]ethyl]acetamide Chemical compound C1N(CC2)CCC2[C@H]1NC1=C(C=2NC3=CC=CC=C3N=2)C(=O)NC2=C1C=C(F)C(NCCNC(=O)C)=C2 TVOCUVRCGNRVTP-QHCPKHFHSA-N 0.000 description 1
- TVOCUVRCGNRVTP-HSZRJFAPSA-N n-[2-[[4-[[(3s)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-6-fluoro-2-oxo-1h-quinolin-7-yl]amino]ethyl]acetamide Chemical compound C1N(CC2)CCC2[C@@H]1NC1=C(C=2NC3=CC=CC=C3N=2)C(=O)NC2=C1C=C(F)C(NCCNC(=O)C)=C2 TVOCUVRCGNRVTP-HSZRJFAPSA-N 0.000 description 1
- OKGNNALOCPMKRB-MHZLTWQESA-N n-[3-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-2-oxo-1h-quinolin-7-yl]phenyl]acetamide Chemical compound CC(=O)NC1=CC=CC(C=2C=C3NC(=O)C(C=4NC5=CC=CC=C5N=4)=C(N[C@@H]4C5CCN(CC5)C4)C3=CC=2)=C1 OKGNNALOCPMKRB-MHZLTWQESA-N 0.000 description 1
- MKWCKCMDTUSNTI-HKBQPEDESA-N n-[3-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-2-oxo-7-piperidin-1-yl-1h-quinolin-6-yl]phenyl]acetamide Chemical compound CC(=O)NC1=CC=CC(C=2C(=CC=3NC(=O)C(C=4NC5=CC=CC=C5N=4)=C(N[C@@H]4C5CCN(CC5)C4)C=3C=2)N2CCCCC2)=C1 MKWCKCMDTUSNTI-HKBQPEDESA-N 0.000 description 1
- NKGYOGQSSWKOBG-PMERELPUSA-N n-[3-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-7-(2-ethylimidazol-1-yl)-2-oxo-1h-quinolin-6-yl]phenyl]acetamide Chemical compound CCC1=NC=CN1C(C(=C1)C=2C=C(NC(C)=O)C=CC=2)=CC2=C1C(N[C@@H]1C3CCN(CC3)C1)=C(C=1NC3=CC=CC=C3N=1)C(=O)N2 NKGYOGQSSWKOBG-PMERELPUSA-N 0.000 description 1
- CDQSFCCLRXEQRC-PMERELPUSA-N n-[3-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-7-(2-methylimidazol-1-yl)-2-oxo-1h-quinolin-6-yl]phenyl]acetamide Chemical compound CC(=O)NC1=CC=CC(C=2C(=CC=3NC(=O)C(C=4NC5=CC=CC=C5N=4)=C(N[C@@H]4C5CCN(CC5)C4)C=3C=2)N2C(=NC=C2)C)=C1 CDQSFCCLRXEQRC-PMERELPUSA-N 0.000 description 1
- FKJPMYPNHOIDPN-NDEPHWFRSA-N n-[3-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-7-(dimethylamino)-2-oxo-1h-quinolin-6-yl]phenyl]acetamide Chemical compound CN(C)C1=CC=2NC(=O)C(C=3NC4=CC=CC=C4N=3)=C(N[C@@H]3C4CCN(CC4)C3)C=2C=C1C1=CC=CC(NC(C)=O)=C1 FKJPMYPNHOIDPN-NDEPHWFRSA-N 0.000 description 1
- ATZGGEASZDTJFM-MHZLTWQESA-N n-[3-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-7-fluoro-2-oxo-1h-quinolin-6-yl]phenyl]acetamide Chemical compound CC(=O)NC1=CC=CC(C=2C(=CC=3NC(=O)C(C=4NC5=CC=CC=C5N=4)=C(N[C@@H]4C5CCN(CC5)C4)C=3C=2)F)=C1 ATZGGEASZDTJFM-MHZLTWQESA-N 0.000 description 1
- GFXMILNSSGCOQJ-LJAQVGFWSA-N n-[3-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-7-imidazol-1-yl-2-oxo-1h-quinolin-6-yl]phenyl]acetamide Chemical compound CC(=O)NC1=CC=CC(C=2C(=CC=3NC(=O)C(C=4NC5=CC=CC=C5N=4)=C(N[C@@H]4C5CCN(CC5)C4)C=3C=2)N2C=NC=C2)=C1 GFXMILNSSGCOQJ-LJAQVGFWSA-N 0.000 description 1
- LRXDIWDWOFFAPX-MHZLTWQESA-N n-[3-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-7-methoxy-2-oxo-1h-quinolin-6-yl]phenyl]acetamide Chemical compound COC1=CC=2NC(=O)C(C=3NC4=CC=CC=C4N=3)=C(N[C@@H]3C4CCN(CC4)C3)C=2C=C1C1=CC=CC(NC(C)=O)=C1 LRXDIWDWOFFAPX-MHZLTWQESA-N 0.000 description 1
- BTVUAVJHMGLJOP-VWLOTQADSA-N n-[3-[4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-imidazo[4,5-b]pyridin-2-yl)-2-oxo-1h-quinolin-6-yl]phenyl]acetamide Chemical compound CC(=O)NC1=CC=CC(C=2C=C3C(N[C@@H]4C5CCN(CC5)C4)=C(C=4NC5=NC=CC=C5N=4)C(=O)NC3=CC=2)=C1 BTVUAVJHMGLJOP-VWLOTQADSA-N 0.000 description 1
- ATZGGEASZDTJFM-HHHXNRCGSA-N n-[3-[4-[[(3s)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-7-fluoro-2-oxo-1h-quinolin-6-yl]phenyl]acetamide Chemical compound CC(=O)NC1=CC=CC(C=2C(=CC=3NC(=O)C(C=4NC5=CC=CC=C5N=4)=C(N[C@H]4C5CCN(CC5)C4)C=3C=2)F)=C1 ATZGGEASZDTJFM-HHHXNRCGSA-N 0.000 description 1
- NMRSTGMHZQSLNU-YTTGMZPUSA-N n-[3-[7-(3-acetylpyrrol-1-yl)-4-[[(3r)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1h-benzimidazol-2-yl)-2-oxo-1h-quinolin-6-yl]phenyl]acetamide Chemical compound CC(=O)NC1=CC=CC(C=2C(=CC=3NC(=O)C(C=4NC5=CC=CC=C5N=4)=C(N[C@@H]4C5CCN(CC5)C4)C=3C=2)N2C=C(C=C2)C(C)=O)=C1 NMRSTGMHZQSLNU-YTTGMZPUSA-N 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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| PCT/US2005/005316 WO2005082340A2 (en) | 2004-02-20 | 2005-02-18 | Modulation of inflammatory and metastatic processes |
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| KR101224410B1 (ko) * | 2003-11-07 | 2013-01-23 | 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 | 퀴놀리논 화합물을 합성하는 방법 |
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| GB0415746D0 (en) | 2004-07-14 | 2004-08-18 | Novartis Ag | Organic compounds |
| US8404718B2 (en) | 2005-01-21 | 2013-03-26 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors |
| AR054425A1 (es) | 2005-01-21 | 2007-06-27 | Astex Therapeutics Ltd | Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico. |
| WO2006077428A1 (en) * | 2005-01-21 | 2006-07-27 | Astex Therapeutics Limited | Pharmaceutical compounds |
| KR101387985B1 (ko) * | 2005-01-27 | 2014-04-25 | 노바티스 백신즈 앤드 다이아그노스틱스 인코포레이티드 | 전이 종양의 치료 |
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| PL1888556T3 (pl) * | 2005-05-17 | 2012-03-30 | Novartis Ag | Metody syntetyzowania związków heterocyklicznych |
| RU2425041C2 (ru) * | 2005-05-23 | 2011-07-27 | Новартис Аг | Кристаллические и другие формы солей, образованных из молочной кислоты и 4-амино-5-фтор-3-[6-(4-метилпиперазин-1-ил)-1н-бензимидазол-2-ил]-1н-хинолин-2-она |
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| US8138205B2 (en) | 2006-07-07 | 2012-03-20 | Kalypsys, Inc. | Heteroarylalkoxy-substituted quinolone inhibitors of PDE4 |
| JP5280357B2 (ja) | 2006-07-07 | 2013-09-04 | スティーブン・ピー・ガベック | Ｐｄｅ４の二環式ヘテロアリール阻害剤 |
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| JP2011526928A (ja) * | 2008-07-03 | 2011-10-20 | ノバルティス アーゲー | 溶融造粒方法 |
| TWI410418B (zh) | 2009-04-29 | 2013-10-01 | Ind Tech Res Inst | 氮雜薁化合物、藥學組合物與抑制一細胞中蛋白質激酶之活性的方法 |
| CA2780031A1 (en) * | 2009-11-12 | 2011-05-19 | Selvita S.A. | A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent |
| TR201819653T4 (tr) * | 2010-04-16 | 2019-01-21 | Novartis Ag | Karaciğer kanserinin tedavisinde kullanılmaya yönelik organik bileşik. |
| RU2430371C1 (ru) * | 2010-04-26 | 2011-09-27 | Учреждение Российской академии наук Институт ядерной физики им. Г.И. Будкера Сибирского отделения РАН (ИЯФ СО РАН) | Способ дифференциальной диагностики и прогноза миомы и рака эндометрия |
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| HK1217092A1 (zh) | 2013-02-15 | 2016-12-23 | Kala Pharmaceuticals, Inc. | 治疗性化合物及其用途 |
| CN105189462B (zh) | 2013-02-20 | 2017-11-10 | 卡拉制药公司 | 治疗性化合物和其用途 |
| US9688688B2 (en) | 2013-02-20 | 2017-06-27 | Kala Pharmaceuticals, Inc. | Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof |
| SG10201704327RA (en) | 2013-10-14 | 2017-06-29 | Eisai R&D Man Co Ltd | Selectively substituted quinoline compounds |
| MX363708B (es) | 2013-10-14 | 2019-03-29 | Eisai R&D Man Co Ltd | Compuestos de quinolina selectivamente sustituidos. |
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| US9890173B2 (en) | 2013-11-01 | 2018-02-13 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| CN104529894B (zh) * | 2015-01-15 | 2017-02-22 | 成都丽凯手性技术有限公司 | 一种喹啉酮类衍生物及其制备方法 |
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| CA3036336A1 (en) | 2016-09-08 | 2018-03-15 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
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| GB201705263D0 (en) * | 2017-03-31 | 2017-05-17 | Probiodrug Ag | Novel inhibitors |
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- 2005-02-18 CN CN2005800095231A patent/CN1960731B/zh not_active Expired - Fee Related
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- 2005-02-18 JP JP2006554253A patent/JP5019884B2/ja not_active Expired - Fee Related
- 2005-02-18 EP EP05723338A patent/EP1718306A2/en not_active Withdrawn
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| WO2002022598A1 (en) * | 2000-09-11 | 2002-03-21 | Chiron Corporation | Quinolinone derivatives as tyrosine kinase inhibitors |
| WO2003087095A1 (en) * | 2002-04-05 | 2003-10-23 | Chiron Corporation | Quinolinone derivatives |
Also Published As
| Publication number | Publication date |
|---|---|
| CA2556872A1 (en) | 2005-09-09 |
| AU2005216904A1 (en) | 2005-09-09 |
| JP5019884B2 (ja) | 2012-09-05 |
| CA2556872C (en) | 2015-05-12 |
| RU2006133536A (ru) | 2008-03-27 |
| US20050239825A1 (en) | 2005-10-27 |
| EP1718306A2 (en) | 2006-11-08 |
| US7875624B2 (en) | 2011-01-25 |
| WO2005082340A2 (en) | 2005-09-09 |
| WO2005082340A3 (en) | 2006-05-04 |
| RU2377988C2 (ru) | 2010-01-10 |
| AU2005216904B2 (en) | 2010-11-25 |
| JP2007523185A (ja) | 2007-08-16 |
| CN1960731A (zh) | 2007-05-09 |
| BRPI0507891A (pt) | 2007-07-24 |
| IL177574A0 (en) | 2006-12-10 |
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